硒鎓胆碱的选定药效学和生化特性。

Selected pharmacodynamic and biochemical properties of selenonium choline.

Khatri J N, Silks L A, Kosh J W

College of Pharmacy, University of South Carolina, Columbia 29208, USA.

Gen Pharmacol. 1998 Jan;30(1):95-101. doi: 10.1016/s0306-3623(97)00080-3.

Abstract

Five minutes after intravenous administration of 50 mg/kg of the novel choline analogue selenonium choline [(CH3)2Se + CH2CH2OH, SeCh], only 8% of the administered dose was accounted for in blood, brain, liver, heart, and kidney tissues. 2. SeCh was acetylated in vivo to acetylselenonium choline (ASeCh) in all of the tissues examined. 3. During postmortem incubation, brain concentrations of SeCh and ASeCh increased to 535% and to 425%, respectively. 4. K(m) and Vmax values for the phosphorylation of SeCh by choline kinase were higher and lower, respectively, compared to the phosphorylation of choline. 5. Acetylation of SeCh was described with K(m) and Vmax values that were both higher than the values for Ch. 6. The data suggest that SeCh is phosphorylated and incorporated into various lipids in brain tissue, and is acetylated to ASeCh by both nonneural and neural tissues.

摘要

静脉注射50毫克/千克新型胆碱类似物硒鎓胆碱[（CH3）2Se + CH2CH2OH，SeCh] 5分钟后，血液、脑、肝、心和肾组织中仅占给药剂量的8%。2. 在所有检测的组织中，SeCh在体内被乙酰化为乙酰硒鎓胆碱（ASeCh）。3. 在死后孵育期间，脑中SeCh和ASeCh的浓度分别增加到535%和425%。4. 与胆碱磷酸化相比，胆碱激酶对SeCh磷酸化的K（m）值较高，Vmax值较低。5. SeCh的乙酰化描述中，K（m）和Vmax值均高于Ch的值。6. 数据表明，SeCh在脑组织中被磷酸化并掺入各种脂质中，并且被非神经组织和神经组织乙酰化为ASeCh。